| Description | IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM. |
| In vitro | IRAK4-IN-1的体外代谢稳定性特征已测定，其在大鼠全血(RWB)中的EC50值为2300 nM。 |
| In vivo | 口服药代动力学研究表明，IRAK4-IN-1具有高生物利用度，为73%，并且其血浆清除率较低（Clp=22 mL/min/kg），从而导致了相对合理的半衰期，为1.3小时。 |
| Animal experiments | In the TLR driven in vivo model, female Lewis rats are dosed with either vehicle or IRAK4-IN-1 (Compound 23; 3, 10, 30, and 100 mg/kg; p.o.) dosed at 1 h prior to stimulation with Resiquimod, R848 (5 mg/kg, IP). At 1.5 h post R848 stimulation, blood samples are obtained from the animals and cytokine levels are measured. |
| Target activity | IRAK4:7 nM. |
| molecular weight | 337.42 |
| Molecular formula | C19H23N5O |
| CAS | 1820787-94-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 1 mg/ml, Sonication is recommended. H2O: < 0.1 mg/mL (insoluble) |
| References | 1. Smith GF, et al. Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2721-2726. |